• Biomolecules & Therapeutics
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• 제22권5호
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• pp.390-399
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• 2014

Chalcones (1,3-diaryl-2-propen-1-ones), a flavonoid subfamily, are widely known for their anti-inflammatory properties. Propenone moiety in chalcones is known to play an important role in generating biological responses by chalcones. In the present study, we synthesized chalcone derivatives structurally modified in propenone moiety and examined inhibitory effect on nitric oxide (NO) production and its potential mechanisms. Among the chalcone derivatives used for this study, TI-I-174 (3-(2-Hydroxyphenyl)-1-(thiophen-3-yl)prop-2-en-1-one) most potently inhibited lipopolysaccharide (LPS)-stimulated nitrite production in RAW 264.7 macrophages. TI-I-174 treatment also markedly inhibited inducible nitric oxide synthase (iNOS) expression. However, TI-I-174 did not significantly affect production of IL-6, cyclooxygenase-2 (COX-2) and tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$), implying that TI-I-174 inhibits production of inflammatory mediators in a selective manner. Treatment of macrophages with TI-I-174 significantly inhibited transcriptional activity of activator protein-1 (AP-1) as determined by luciferase reporter gene assay, whereas nuclear factor-${\kappa}B$ (NF-${\kappa}B$) activity was not affected by TI-I-1744. In addition, TI-I-174 significantly inhibited activation of c-Jun-N-Terminal kinase (JNK) without affecting ERK1/2 and p38MAPK, indicating that down-regulation of iNOS gene expression by TI-I-174 is mainly attributed by blockade of JNK/AP-1 activation. We also demonstrated that TI-I-174 treatment led to an increase in heme oxygenase-1 (HO-1) expression both at mRNA and protein level. Transfection of siRNA targeting HO-1 reversed TI-I-174-mediated inhibition of nitrite production. Taken together, these results indicate that TI-I-174 suppresses NO production in LPS-stimulated RAW 264.7 macrophages via induction of HO-1 and blockade of AP-1 activation.

• Asian Pacific Journal of Cancer Prevention
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• 제14권10호
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• pp.5783-5788
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• 2013

Trigonella foenum in graecum (Fenugreek) is a traditional herbal plant used to treat disorders like diabetes, high cholesterol, wounds, inflammation, gastrointestinal ailments, and it is believed to have anti-tumor properties, although the mechanisms for the activity remain to be elucidated. In this study, we prepared a methanol extract from Fenugreek whole plants and investigated the mechanism involved in its growth-inhibitory effect on MCF-7 human breast cancer cells. Apoptosis of MCF-7 cells was evidenced by investigating trypan blue exclusion, TUNEL and Caspase 3, 8, 9, p53, FADD, Bax and Bak by real-time PCR assays inducing activities, in the presence of FME at $65{\mu}g/mL$ for 24 and 48 hours. FME induced apoptosis was mediated by the death receptor pathway as demonstrated by the increased level of Fas receptor expression after FME treatment. However, such change was found to be absent in Caspase 3, 8, 9, p53, FADD, Bax and Bak, which was confirmed by a time-dependent and dose-dependent manner. In summary, these data demonstrate that at least 90% of FME induced apoptosis in breast cell is mediated by Fas receptor-independently of either FADD, Caspase 8 or 3, as well as p53 interdependently.

• 생약학회지
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• 제43권3호
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• pp.217-223
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• 2012

In the present study, we investigated anti-inflammatory activity of artemisinic acid in HaCaT cells and RAW264.7 cells. Artemisinic acid showed inhibitory activity on macrophage-derived chemokines (MDC) expression, a factor related with atopic dermatitis (AD), in interferon (IFN)-${\gamma}$ and tumor necrosis factor (TNF)-${\alpha}$-stimulated HaCaT cells. In the study on action mechanism, pretreated artemisinic acid reduced the phosphorylation of STAT1 and p38 and the degradation of $I{\kappa}B$ by IFN-${\gamma}$ and TNF-${\alpha}$ stimulations. However, artemisinic acid didn't show the inhibitory activity on LPS-induced inflammatory mediators (NO, $PGE_2$, IL-6) in RAW264.7 cell. These results indicate that artemisinic acid inhibits IFN-${\gamma}$ and TNF-${\alpha}$-induced MDC expression through inhibition of signal factors, STAT1, NF-${\kappa}B$, and p38, in HaCaT keratinocytes.

• 동의생리병리학회지
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• 제30권5호
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• pp.338-346
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• 2016

Signal transducer and activator of transcription 3 (STAT3) is associated with various human diseases, such as cancer, auto-immune disease, and intestinal inflammation. The limited and inadequate effect of standard approaches for treating inflammatory bowel disease (IBD) has prompted to develop alternative anti-colitis agents through inhibition of STAT3. Here, we show that gallic acid (GA), a 3,4,5-trihydroxybenzoic acid, markedly reduced phosphorylation of STAT3. Among the derivatives of benzoic acids, GA showed significant inhibition on STAT3 phosphorylation. In addition, GA ameliorated the dextran sodium sulfate (DSS)-induced acute colitis as determined by the measurement of symptomatic and histological indices. The suppression of DSS-induced acute colitis by GA treatment may be related to the regulation of cytokines and growth factors. Furthermore, GA inhibited phosphorylation of STAT3 in the colon tissue of DSS-treated mice. These findings may be useful in comprehending the molecular action of GA on STAT3 phosphorylation and provide novel insights into the potential application of GA in the treatment of STAT3-related inflammatory disease, such as IBD.

• 생명과학회지
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• 제15권2호
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• pp.279-286
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• 2005

손바닥선인장 추출물은 한의학에서 항염증 작용, 화상, 부종, 소화 불량 등 몇 가지의 생리학적 기능이 확인되었다. 본 연구에서는 손바닥선인장 줄기를 메탄올을 이용하여 추출한 후 그 추출물을 이용하여 항균활성을 확인한 결과 병원균 등 일반 세균에서 항균활성을 확인하였다. 특히, 약제내성균 및 혐기성 균인 여드름 원인균 뿐만 아니라 효모, 곰팡이 등 진균류에서도 항균활성을 나타내어 넓은 항균 스펙트럼을 가지고 있음을 확인할 수 있었다. 또한 열 처리, 저장온도 및 저장기간이 항균활성에 영향을 미치지 않았으므로 온도 및 기간에 안정함을 확인할 수 있었고, 식품 보존제로서의 가능성 확인 시험에서도 기존의 식품 보존제보다 안전성이 있는 항균활성 물질로 평가되었다.

• Biomolecules & Therapeutics
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• 제23권5호
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• pp.421-427
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• 2015

Imperatorin has been known to exert many biological functions including anti-inflammatory activity. In this study, we investigated the inhibitory effects of imperatorin on the production of inflammatory mediators in mouse bone marrow-derived mast cells (BMMC). Imperatorin inhibited degranulation and the generation of eicosanoids (leukotriene $C_4$ ($LTC_4$) and prostaglandin $D_2$ ($PGD_2$) in IgE/antigen (Ag)-stimulated BMMC. To elucidate the molecular mechanism involved in this process, we investigated the effect of imperatorin on intracellular signaling in BMMC. Biochemical analyses of the IgE/Ag-mediated signaling pathway demonstrated that imperatorin dramatically attenuated degranulation and the production of 5-lipoxygenase-dependent $LTC_4$ and cyclooxygenase-2-dependent $PGD_2$ through the inhibition of intracellular calcium influx/phospholipase $C{\gamma}1$, cytosolic phospholipase $A_2$/mitogen-activated protein kinases and/or nuclear factor-${\kappa}B$ pathways in BMMC. These results suggest that the effects of imperatorin on inhibition of degranulation and eicosanoid generation through the suppression of multiple steps of IgE/Ag-mediated signaling pathways would be beneficial for the prevention of allergic inflammation.

• 한방재활의학과학회지
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• 제23권2호
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• pp.17-31
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• 2013

Objectives : Peripheral nerve injuries are commonly encountered clinical problems and often result in serve functional deficit. Bee venom and scolopendra subspinipes have been traditionally used in oriental medicine to treat several inflammatory diseases and chronic pain conditions. Methods : In the present study, the effects of bee venom pharmacopuncture and scolopendra subspinipes pharmacopuncture on functional recovery, severity of pain, and expressions of neurofilament, cycloxygenease-2(COX-2), and tumor necrosis factor-${\alpha}$(TNF-${\alpha}$) following sciatic crushed nerve injury in rats were investigated. For this study, walking tract analysis, plantar test, western blot for COX-2 and TNF-${\alpha}$, and immunohistochemistry for neurofilament were performed. Results : In the present results, sciatic functional index(SFI) in walking tract analysis was significantly decreased following sciatic crushed nerve injury, and pain severity in plantar test was significantly increased. COX-2 and TNF-${\alpha}$ expressions were increased whereas neurofilament expression was decreased by sciatic crushed nerve injury. On the other hand, bee venom pharmacopuncture and scolopendra subspinipes pharmacopuncture improved SFI in walking tract analysis and suppressed the pain severity in sciatic crushed nerve injury. Bee venom pharmacopuncture and scolopendra subspinipes pharmacopuncture suppressed COX-2 and TNF-${\alpha}$ expression and enhanced the neurofilament expression in sciatic crushed nerve injury. Conclusions : In the present study, we have shown that treatment with bee venom or scolopendra subspinipes is the effective therapeutic modality to ameliorate the symptoms of sciatic crushed nerve injury. The efficacies of bee venom and scolopendra subspinipes were similar.

• 약학회지
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• 제53권6호
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• pp.321-327
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• 2009

Licochalcone A is a chalcone isolated from the roots of Glycyrrhiza inflate. In this study, we examined the effects of licochalonce A on the production of cytokines in LPS-activated macrophages. Licochalcone A inhibited the secretion of proinflammatory cytokines such as IL-1$\beta$, IL-6, and TNF-$\alpha$. The reduced secretion of proinflammatory cytokines is related to the differences in the mRNA expression of IL-1$\beta$, IL-6, and TNF-$\alpha$. Moreover, licochalcone A inhibited the mRNA expression of IL-12p40, IL-18, and IL-23p19. To investigate its mechanism, we performed gel shift assay. Licochalcone A reduced nuclear NF-${\kappa}B$ binding activity in LPS-activated RAW264.7 cells. Taken together, these results suggest that licochalcone A has anti-inflammatory effects in LPS-activated macrophages and its mechanism could be through the down-regulation of binding to the ${\kappa}B$ site.

• 혜화의학회지
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• 제20권2호
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• pp.125-131
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• 2012

알레르기성 접촉 피부염을 진단 받고 양방치료를 받았으나 별무 호전하던 환자에게 침치료와 양격산가감방을 복용하여 약 2개월간 증상이 초기보다 증상이 완화되는 효과가 있었다. 그러나 약물 치료를 배제하고 침치료만 시행하던 중 환자가 상열감 및 소양감은 거의 소실되었으나 홍조 증상이 정체 양상을 보였고 이에 저자는 치료후기를 혈조 상태로 변증하고 환자의 환부에 경피적외선조사요법을 시행하여 정체중이던 안면홍조 상태가 최근 약 1달간 10회의 치료로 환자가 만족할만한 효과가 있었다.

• Journal of Ginseng Research
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• 제44권4호
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• pp.655-663
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• 2020

Background: Korean Red Ginseng is known to exhibit immune-enhancing and anti-inflammatory properties. The immune-enhancing effects of the nonsaponin fraction (NSF) of Korean Red Ginseng have been studied in many reports. However, the gastroprotective effect of this fraction is not fully understood. In this study, we demonstrate the activities of NSF for gastrointestinal protection and its related critical factor. Methods: The in vitro and in vivo regulatory functions of NSF on cyclooxygenase-1 (COX-1) messenger RNA and protein levels were examined by reverse transcription polymerase chain reaction and immunoblotting analyses. Gastroprotective effects of NSF were investigated by histological score, gastric juice pH, and myeloperoxidase activity on indomethacin-induced, cold stress-induced, and acetylsalicylic acid-induced gastritis and dextran sulfate sodium-induced colitis in in vivo mouse models. Results: NSF did not show cytotoxicity, and it increased COX-1 messenger RNA expression and protein levels in RAW264.7 cells. This upregulation was also observed in colitis and gastritis in vivo models. In addition, NSF treatment in mice ameliorated the symptoms of gastrointestinal inflammation, including histological score, colon length, gastric juice pH, gastric wall thickness, and myeloperoxidase activity. Conclusion: These results suggest that NSF has gastroprotective effects on gastritis and colitis in in vivo mouse models through COX-1 upregulation.